JP3761781B2 - 不安定なdpiv阻害剤の化合物 - Google Patents

不安定なdpiv阻害剤の化合物 Download PDF

Info

Publication number
JP3761781B2
JP3761781B2 JP2000555930A JP2000555930A JP3761781B2 JP 3761781 B2 JP3761781 B2 JP 3761781B2 JP 2000555930 A JP2000555930 A JP 2000555930A JP 2000555930 A JP2000555930 A JP 2000555930A JP 3761781 B2 JP3761781 B2 JP 3761781B2
Authority
JP
Japan
Prior art keywords
compound
pro
inhibitor
dipeptidyl
inhibitors
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2000555930A
Other languages
English (en)
Japanese (ja)
Other versions
JP2002518518A (ja
Inventor
デムート,ハンス−ウルリッヒ
シュミット,イェルン
ホフマン,トルステン
グルント,コンラッド
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Prosidion Ltd
Original Assignee
Prosidion Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Prosidion Ltd filed Critical Prosidion Ltd
Publication of JP2002518518A publication Critical patent/JP2002518518A/ja
Application granted granted Critical
Publication of JP3761781B2 publication Critical patent/JP3761781B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2000555930A 1998-06-24 1999-06-24 不安定なdpiv阻害剤の化合物 Expired - Fee Related JP3761781B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19828114A DE19828114A1 (de) 1998-06-24 1998-06-24 Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19828114.5 1998-06-24
PCT/EP1999/004381 WO1999067279A1 (de) 1998-06-24 1999-06-24 Verbindungen von instabilen dp iv-inhibitoren

Publications (2)

Publication Number Publication Date
JP2002518518A JP2002518518A (ja) 2002-06-25
JP3761781B2 true JP3761781B2 (ja) 2006-03-29

Family

ID=7871860

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2000555930A Expired - Fee Related JP3761781B2 (ja) 1998-06-24 1999-06-24 不安定なdpiv阻害剤の化合物

Country Status (17)

Country Link
US (1) US7053055B2 (no)
EP (1) EP1090030A1 (no)
JP (1) JP3761781B2 (no)
KR (1) KR100630254B1 (no)
CN (1) CN100345866C (no)
AU (1) AU758843B2 (no)
BR (1) BR9911415A (no)
CA (1) CA2335978A1 (no)
DE (1) DE19828114A1 (no)
HU (1) HUP0102250A3 (no)
IL (1) IL140338A0 (no)
IS (1) IS5739A (no)
NO (1) NO20006483L (no)
NZ (1) NZ508721A (no)
PL (1) PL345060A1 (no)
RU (1) RU2226195C2 (no)
WO (1) WO1999067279A1 (no)

Families Citing this family (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020006899A1 (en) * 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
DE69837393T2 (de) * 1997-09-29 2007-12-06 Point Therapeutics, Inc., Boston Stimulierung von hämatopoietischen zellen im vitro
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
US20030176357A1 (en) * 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
US6890904B1 (en) * 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
WO2001034594A1 (en) * 1999-11-12 2001-05-17 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
EP1259246A2 (en) * 2000-02-25 2002-11-27 Novo Nordisk A/S Use of dpp-iv inhibitors for the treatment of diabetes
US6395767B2 (en) * 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
EP2266665B1 (en) 2000-03-31 2016-05-11 Royalty Pharma Collection Trust Method for the improvement of islet signaling in diabetes mellitus and for its prevention
EP1891948A1 (en) 2000-10-27 2008-02-27 Probiodrug AG Treatment of neurological and neuropsychological disorders
CA2433090A1 (en) * 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
ATE353900T1 (de) * 2001-02-24 2007-03-15 Boehringer Ingelheim Pharma Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
AU2002254567B2 (en) 2001-04-11 2007-10-11 Bristol-Myers Squibb Company Amino acid complexes of C-aryl glucosides for treatment of diabetes and method
US20030060494A1 (en) * 2001-05-18 2003-03-27 Nobuyuki Yasuda Pharmaceutical use of N-carbamoylazole derivatives
CN1723196A (zh) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
DE10150203A1 (de) * 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
UA74912C2 (en) * 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
IL160917A0 (en) 2001-10-18 2004-08-31 Bristol Myers Squibb Co Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions
US7238671B2 (en) 2001-10-18 2007-07-03 Bristol-Myers Squibb Company Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions
CA2468192A1 (en) * 2001-11-26 2003-06-05 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
MXPA04007252A (es) 2002-01-29 2005-03-31 Wyeth Corp Composiciones y metodos para modular los hemicanales de conexina.
EP1338595B1 (en) 2002-02-25 2006-05-03 Eisai Co., Ltd. Xanthine derivatives as DPP-IV inhibitors
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
CN101273987A (zh) * 2002-06-03 2008-10-01 诺瓦提斯公司 取代的氰基吡咯烷和含有它们的组合制剂用于治疗高脂血症和相关疾病的用途
CA2491466A1 (en) * 2002-07-09 2004-01-15 Sharlene Adams Methods and compositions relating to isoleucine boroproline compounds
EP1528931B1 (en) 2002-08-09 2008-05-07 Prosidion Ltd. Dipeptidyl peptidase iv inhibitors for decreasing the rate of chronic weight gain
CA2496249C (en) * 2002-08-21 2012-01-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-amino-piperidin-1-yl]-xanthines, the production thereof and the use of the same as medicaments
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
ES2344057T3 (es) 2002-10-23 2010-08-17 Bristol-Myers Squibb Company Inhibidores de la dipeptidil peptidasa iv basados en nitrilos de glicina.
US7098235B2 (en) 2002-11-14 2006-08-29 Bristol-Myers Squibb Co. Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds
TW200504021A (en) 2003-01-24 2005-02-01 Bristol Myers Squibb Co Substituted anilide ligands for the thyroid receptor
US7148246B2 (en) 2003-02-27 2006-12-12 Sanofi-Aventis Deutschland Gmbh Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals
DE10308351A1 (de) 2003-02-27 2004-11-25 Aventis Pharma Deutschland Gmbh 1,3-substituierte Cycloalkylderivate mit sauren, meist heterocyclischen Gruppen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE10308355A1 (de) 2003-02-27 2004-12-23 Aventis Pharma Deutschland Gmbh Aryl-cycloalkyl substituierte Alkansäurederivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel
DE10308352A1 (de) 2003-02-27 2004-09-09 Aventis Pharma Deutschland Gmbh Arylcycloalkylderivate mit verzweigten Seitenketten, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel
DE10308353A1 (de) 2003-02-27 2004-12-02 Aventis Pharma Deutschland Gmbh Diarylcycloalkylderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7687625B2 (en) 2003-03-25 2010-03-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
PT1620082E (pt) 2003-05-05 2010-06-11 Probiodrug Ag Utilização médica de inibidores de ciclases de glutaminilo e glutamato para o tratamento da doença de alzheimer e síndrome de down
EP1620091B1 (en) 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
EA009291B1 (ru) 2003-05-05 2007-12-28 Пробиодруг Аг Применение эффекторов глутаминил- и глутаматциклаз
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7459474B2 (en) 2003-06-11 2008-12-02 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
BRPI0413452A (pt) 2003-08-13 2006-10-17 Takeda Pharmaceutical composto, composição farmacêutica, kit, artigo de fabricação, e, métodos de inibir dpp-iv, terapêutico e de tratar um estado de doença, cáncer, distúrbios autoimunes, uma condição einfecção por hiv
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP5707014B2 (ja) 2003-10-15 2015-04-22 プロビオドルグ エージー グルタミニル、及びグルタミン酸シクラーゼのエフェクターの使用
EP1677758A1 (en) * 2003-10-31 2006-07-12 ALZA Corporation Compositions and dosage forms for enhanced absorption of 3-amino-n-butyl-phosphinic acid
EP1824846A2 (en) 2003-11-03 2007-08-29 Probiodrug AG Novel compounds for the treatment of neurological disorders
NZ546887A (en) 2003-11-03 2009-04-30 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
MXPA06005518A (es) 2003-11-17 2006-08-17 Novartis Ag Uso de inhibidores de la dipeptidil peptidasa iv.
WO2005067976A2 (en) 2004-01-20 2005-07-28 Novartis Ag Direct compression formulation and process
US7241787B2 (en) 2004-01-25 2007-07-10 Sanofi-Aventis Deutschland Gmbh Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
KR101099206B1 (ko) 2004-02-05 2011-12-27 프로비오드룩 아게 신규한 글루타미닐 시클라제 저해제
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AU2004318013B8 (en) 2004-03-15 2011-10-06 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1586573B1 (en) 2004-04-01 2007-02-07 Sanofi-Aventis Deutschland GmbH Oxadiazolones, processes for their preparation and their use as pharmaceuticals
WO2005118555A1 (en) 2004-06-04 2005-12-15 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7145040B2 (en) 2004-07-02 2006-12-05 Bristol-Myers Squibb Co. Process for the preparation of amino acids useful in the preparation of peptide receptor modulators
TW200611704A (en) 2004-07-02 2006-04-16 Bristol Myers Squibb Co Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions
US7534763B2 (en) 2004-07-02 2009-05-19 Bristol-Myers Squibb Company Sustained release GLP-1 receptor modulators
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7842707B2 (en) * 2004-07-23 2010-11-30 Nuada, Llc Peptidase inhibitors
US20060063719A1 (en) * 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
AR051446A1 (es) 2004-09-23 2007-01-17 Bristol Myers Squibb Co Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2)
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
EP2805953B1 (en) 2004-12-21 2016-03-09 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2006068480A2 (en) * 2004-12-23 2006-06-29 Campina Nederland Holding B.V. Protein hydrolysate enriched in peptides inhibiting dpp-iv and their use
US7635699B2 (en) 2004-12-29 2009-12-22 Bristol-Myers Squibb Company Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods
US7589088B2 (en) 2004-12-29 2009-09-15 Bristol-Myers Squibb Company Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods
DOP2006000008A (es) * 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
US7317024B2 (en) 2005-01-13 2008-01-08 Bristol-Myers Squibb Co. Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
EP2527337A1 (en) 2005-04-14 2012-11-28 Bristol-Myers Squibb Company Inhibitors of 11-beta hydroxysteroid dehydrogenase type I
US7521557B2 (en) 2005-05-20 2009-04-21 Bristol-Myers Squibb Company Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
US20090317376A1 (en) 2005-06-06 2009-12-24 Georgetown University Medical School Compositions And Methods For Lipo Modeling
DE102005026762A1 (de) 2005-06-09 2006-12-21 Sanofi-Aventis Deutschland Gmbh Azolopyridin-2-on-derivate als Inhibitoren von Lipasen und Phospholipasen
US7888381B2 (en) 2005-06-14 2011-02-15 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
CA2617715A1 (en) * 2005-08-11 2007-02-15 F. Hoffmann-La Roche Ag Pharmaceutical composition comprising a dpp-iv inhibitor
EP1942898B2 (en) 2005-09-14 2014-05-14 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors for treating diabetes
JP5122462B2 (ja) 2005-09-16 2013-01-16 武田薬品工業株式会社 ジペプチジルペプチダーゼ阻害剤
EP1943215A2 (en) 2005-10-31 2008-07-16 Brystol-Myers Squibb Company Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase iv and methods
WO2007054577A1 (en) 2005-11-14 2007-05-18 Probiodrug Ag Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase iv inhibitors
JP2009517464A (ja) 2005-11-30 2009-04-30 カンピーナ ネーダーランド ホールディング ビー.ブイ. グルカゴン様ペプチド1の活性を増強するタンパク質加水分解物の使用
US7592461B2 (en) 2005-12-21 2009-09-22 Bristol-Myers Squibb Company Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
KR101281962B1 (ko) 2006-04-11 2013-07-08 아레나 파마슈티칼스, 인크. 특정 개체에게서 골 질량을 증가시키는 데에 유용한 화합물을 확인하기 위해 gpr119 수용체를 사용하는 방법
PE20071221A1 (es) * 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
MX2008013130A (es) 2006-04-12 2008-11-19 Probiodrug Ag Inhibidores de enzima.
CN102838599A (zh) 2006-05-04 2012-12-26 贝林格尔.英格海姆国际有限公司 多晶型
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
PE20080251A1 (es) * 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
US20100022457A1 (en) 2006-05-26 2010-01-28 Bristol-Myers Squibb Company Sustained release glp-1 receptor modulators
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
US7795291B2 (en) 2006-07-07 2010-09-14 Bristol-Myers Squibb Company Substituted acid derivatives useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic and anti-obesity agents and method
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US7968577B2 (en) 2006-11-01 2011-06-28 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
JP2010508358A (ja) 2006-11-01 2010-03-18 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体、AP−1、および/またはNF−κB活性の調節剤、並びにその使用
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
WO2008065141A1 (en) 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
RU2446796C2 (ru) 2006-12-26 2012-04-10 Фармасайкликс, Инк. Способ использования ингибиторов гистондеацетилазы и мониторинга биомаркеров в комбинированной терапии
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
AR065809A1 (es) 2007-03-22 2009-07-01 Bristol Myers Squibb Co Formulaciones farmaceuticas que contienen un inhibidor sglt2
EP2865670B1 (en) 2007-04-18 2017-01-11 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
PE20090696A1 (es) 2007-04-20 2009-06-20 Bristol Myers Squibb Co Formas cristalinas de saxagliptina y procesos para preparar las mismas
CA3089569C (en) 2007-06-04 2023-12-05 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US20100120694A1 (en) 2008-06-04 2010-05-13 Synergy Pharmaceuticals, Inc. Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CN101808995A (zh) 2007-07-27 2010-08-18 百时美施贵宝公司 新颖的葡糖激酶激活剂及其使用方法
NZ600126A (en) * 2007-08-17 2013-12-20 Boehringer Ingelheim Int Purine derivatives for use in the treatment of fap-related diseases
WO2009058944A2 (en) 2007-11-01 2009-05-07 Bristol-Myers Squibb Company Nonsteroidal compounds useful as modulators of glucocorticoid receptor ap-1 and /or nf- kappa b activity and use thereof
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
JP2011525537A (ja) 2008-06-24 2011-09-22 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体、AP−1、および/またはNF−κB活性のシクロペンタチオフェン調節剤およびその使用
EP2321341B1 (en) 2008-07-16 2017-02-22 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
AU2009281122C1 (en) * 2008-08-15 2016-04-21 Boehringer Ingelheim International Gmbh Purin derivatives for use in the treatment of fab-related diseases
AU2009290911A1 (en) 2008-09-10 2010-03-18 Boehringer Ingelheim International Gmbh Combination therapy for the treatment of diabetes and related conditions
JP5781930B2 (ja) * 2008-09-12 2015-09-24 カディラ ファーマシューティカルズ リミテッド 新規なジペプチジルペプチダーゼ(dp−iv)化合物
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
AU2009331471B2 (en) 2008-12-23 2015-09-03 Boehringer Ingelheim International Gmbh Salt forms of organic compound
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
EP2498757A1 (en) 2009-11-13 2012-09-19 Bristol-Myers Squibb Company Reduced mass metformin formulations
SI2498759T1 (sl) 2009-11-13 2018-12-31 Astrazeneca Ab Formulacije tablet s takojšnjim sproščanjem
CA2987757C (en) 2009-11-13 2021-04-13 Astrazeneca Uk Limited Bilayer tablet formulations
KR102668834B1 (ko) 2009-11-27 2024-05-24 베링거 인겔하임 인터내셔날 게엠베하 리나글립틴과 같은 dpp-iv 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
TWI562775B (en) 2010-03-02 2016-12-21 Lexicon Pharmaceuticals Inc Methods of using inhibitors of sodium-glucose cotransporters 1 and 2
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
EP2545047B9 (en) 2010-03-10 2015-06-10 Probiodrug AG Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
ES2559209T3 (es) 2010-04-14 2016-02-11 Bristol-Myers Squibb Company Nuevos activadores de la glucocinasa y métodos de uso de los mismos
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
ES2935300T3 (es) 2010-05-05 2023-03-03 Boehringer Ingelheim Int Combiterapia
KR20230051307A (ko) 2010-06-24 2023-04-17 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
MX2013002146A (es) 2010-09-03 2013-04-03 Astrazeneca Uk Ltd Formulaciones farmaceuticas que utilizan antioxidantes solubles en agua.
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
TWI631963B (zh) 2011-01-05 2018-08-11 雷西肯製藥股份有限公司 包含鈉-葡萄糖共同輸送體1與2之抑制劑的組合物與應用方法
CN103442697A (zh) 2011-02-01 2013-12-11 百时美施贵宝公司 包含胺化合物的药物制剂
CN108676076A (zh) 2011-03-01 2018-10-19 辛纳吉制药公司 制备鸟苷酸环化酶c激动剂的方法
JP6050264B2 (ja) 2011-03-16 2016-12-21 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
EA030121B1 (ru) 2011-07-15 2018-06-29 Бёрингер Ингельхайм Интернациональ Гмбх Замещенные хиназолины, их получение и их применение в фармацевтических композициях
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
WO2013171167A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
DK3489226T3 (da) 2012-11-20 2021-04-26 Lexicon Pharmaceuticals Inc Hæmmere for natriumglucose-cotransporter 1
JP2016514670A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド 他の薬物と組み合わせたグアニル酸シクラーゼ受容体アゴニスト
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
RS65632B1 (sr) 2013-06-05 2024-07-31 Bausch Health Ireland Ltd Ultra-prečišćeni agonisti guanilat-ciklaze c, postupak njihove pripreme i upotrebe
US9593113B2 (en) 2013-08-22 2017-03-14 Bristol-Myers Squibb Company Imide and acylurea derivatives as modulators of the glucocorticoid receptor
ES2950384T3 (es) 2014-02-28 2023-10-09 Boehringer Ingelheim Int Uso médico de un inhibidor de DPP-4
SG10202103552XA (en) 2015-03-09 2021-05-28 Intekrin Therapeutics Inc Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
EP4233840A3 (en) 2016-06-10 2023-10-18 Boehringer Ingelheim International GmbH Combinations of linagliptin and metformin
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
AU2018249822A1 (en) 2017-04-03 2019-10-31 Coherus Biosciences Inc. PPArgamma agonist for treatment of progressive supranuclear palsy
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
SG11202100417RA (en) 2018-07-19 2021-02-25 Astrazeneca Ab Methods of treating hfpef employing dapagliflozin and compositions comprising the same
WO2020068661A1 (en) 2018-09-26 2020-04-02 Lexicon Pharmaceuticals, Inc. Crystalline forms of n-(1 -((2-(dimethylamino)ethyl)amino)-2-m ethyl-1 -oopropan-2-yl)-4-(4-(2-methyl-5- (2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl) phenl)butanamide and methods of their synthesis
EP3871665A1 (en) 2020-02-28 2021-09-01 Martin-Luther-Universität Halle-Wittenberg Inhibitors of rna-binding proteins as anti-cancer drugs
US20220023252A1 (en) 2020-07-27 2022-01-27 Astrazeneca Ab Methods of treating chronic kidney disease with dapagliflozin
CN118510504A (zh) 2022-01-26 2024-08-16 阿斯利康(瑞典)有限公司 用于在治疗糖尿病前期或降低发展2型糖尿病的风险中使用的达格列净

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE296075C (no)
US2961377A (en) 1957-08-05 1960-11-22 Us Vitamin Pharm Corp Oral anti-diabetic compositions and methods
US3174901A (en) 1963-01-31 1965-03-23 Jan Marcel Didier Aron Samuel Process for the oral treatment of diabetes
DE1961686B2 (de) * 1969-12-02 1979-05-31 Siemens Ag, 1000 Berlin Und 8000 Muenchen UEberstromschutzrelais fuer Wechselstromnetze
DE2009743A1 (de) 1970-03-03 1971-09-16 Farbenfabriken Bayer Ag, 5090 Leverkusen Substituierte Biguanide mit antihyperglykämischer Wirkung
US3879541A (en) 1970-03-03 1975-04-22 Bayer Ag Antihyperglycemic methods and compositions
US3960949A (en) 1971-04-02 1976-06-01 Schering Aktiengesellschaft 1,2-Biguanides
CH602612A5 (no) 1974-10-11 1978-07-31 Hoffmann La Roche
US4935493A (en) 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
US5433955A (en) 1989-01-23 1995-07-18 Akzo N.V. Site specific in vivo activation of therapeutic drugs
ATE164852T1 (de) 1990-01-24 1998-04-15 Douglas I Buckley Glp-1-analoga verwendbar in der diabetesbehandlung
ATE148130T1 (de) 1990-04-14 1997-02-15 New England Medical Center Inc Typ-iv-dipeptidyl-aminopeptidase-inhibitoren
US5462928A (en) 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
WO1991017767A1 (en) 1990-05-21 1991-11-28 New England Medical Center Hospitals, Inc. Method of treating inhibition of dipeptidyl aminopeptidase type iv
JPH0819154B2 (ja) 1991-03-14 1996-02-28 江崎グリコ株式会社 ジペプチジルカルボキシペプチダーゼを阻害するペプチド
JPH04334357A (ja) 1991-05-02 1992-11-20 Fujirebio Inc 酵素阻害作用を有するアシル誘導体
EP1050540B1 (en) * 1991-10-22 2006-12-27 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
IL106998A0 (en) 1992-09-17 1993-12-28 Univ Florida Brain-enhanced delivery of neuroactive peptides by sequential metabolism
FR2696740B1 (fr) 1992-10-13 1994-12-30 Dospharma Sa Dérivés prodrogués de la diméthylbiguanide et applications comme médicaments.
WO1995011689A1 (en) * 1993-10-29 1995-05-04 Trustees Of Tufts College Use of inhibitors of dipeptidyl-aminopeptidase to block entry of hiv into cells
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
CA2137206A1 (en) 1993-12-09 1995-06-10 John A. Galloway Glucagon-like insulinotropic peptides, compositions and methods
US5543396A (en) 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
US5614379A (en) 1995-04-26 1997-03-25 Eli Lilly And Company Process for preparing anti-obesity protein
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
WO1997045117A1 (en) 1996-05-29 1997-12-04 Prototek, Inc. Prodrugs of thalidomide and methods for using same as modulators of t-cell function
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
AR016751A1 (es) 1996-11-22 2001-08-01 Athena Neurosciences Inc Metodo para inhibir la liberacion del peptido beta-amiloide en una celula, composicion farmaceutica y compuestos utiles en dicho metodo
AU4854999A (en) 1998-07-02 2000-01-24 Invitro Diagnostics, Inc. Methods, compositions and apparatus for making nucleic acid molecules having a selected affinity to a target molecule
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
AU3960400A (en) 1999-03-05 2000-09-28 Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv
EP1259246A2 (en) 2000-02-25 2002-11-27 Novo Nordisk A/S Use of dpp-iv inhibitors for the treatment of diabetes

Also Published As

Publication number Publication date
RU2226195C2 (ru) 2004-03-27
PL345060A1 (en) 2001-11-19
NO20006483D0 (no) 2000-12-19
EP1090030A1 (de) 2001-04-11
CA2335978A1 (en) 1999-12-29
HUP0102250A3 (en) 2001-12-28
BR9911415A (pt) 2001-03-20
IS5739A (is) 2000-11-28
KR100630254B1 (ko) 2006-10-02
NO20006483L (no) 2000-12-19
DE19828114A1 (de) 2000-01-27
JP2002518518A (ja) 2002-06-25
US20010020006A1 (en) 2001-09-06
CN1306541A (zh) 2001-08-01
NZ508721A (en) 2003-06-30
IL140338A0 (en) 2002-02-10
HUP0102250A2 (hu) 2001-11-28
CN100345866C (zh) 2007-10-31
US7053055B2 (en) 2006-05-30
KR20010071563A (ko) 2001-07-28
WO1999067279A1 (de) 1999-12-29
AU758843B2 (en) 2003-04-03
AU4777299A (en) 2000-01-10

Similar Documents

Publication Publication Date Title
JP3761781B2 (ja) 不安定なdpiv阻害剤の化合物
JP4088419B2 (ja) Dpiv阻害剤のプロドラッグ
US4346078A (en) Novel anticoagulant agmatine derivatives and process for the preparation thereof
EP1245568B1 (fr) Dérives sulfonyles d'-aminoacides et leur utilisation en tant qu'inhibiteurs de dipeptidyl-peptidase IV ( DPP IV)
JP2016147895A (ja) 自己免疫疾患の治療方法及びそれに関する試薬
PT1206485E (pt) Novos efectores da dipeptidil peptidase iv para a utilização tópica
HU194282B (en) Process for preparing novel insulin derivatives modified on c terminal of b chain and pharmaceuticals comprising the same as active substance
JPH03386B2 (no)
MXPA00012215A (en) Compounds of unstable dipeptidyl peptidase iv inhibitors
CZ20004796A3 (cs) Sloučeniny nestabilních DP IV-inhibitorů
MXPA00012217A (en) Prodrugs of dipeptidyl peptidase iv inhibitors
CS277405B6 (en) Peptides with 1-amino-1-cycloalkane carboxylic acid
FR2717391A1 (fr) Peptides pour inhiber la libération de pepsine.
JPH08183740A (ja) 細胞接着阻害剤及び該阻害剤を含む抗炎症剤
CZ20004764A3 (cs) Prekursory DP IV-inhibitorů
JPH11292894A (ja) N−アシルテトラヒドロキノリン誘導体
CH532024A (fr) Procédé de préparation de dérivés de l'insuline

Legal Events

Date Code Title Description
A529 Written submission of copy of amendment under article 34 pct

Free format text: JAPANESE INTERMEDIATE CODE: A529

Effective date: 20001225

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20010215

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20031021

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20040120

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20030903

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20041221

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20050802

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20051101

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20060104

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20060111

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20100120

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110120

Year of fee payment: 5

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120120

Year of fee payment: 6

LAPS Cancellation because of no payment of annual fees